Atrasentan is a potent and selective antagonist for the endothelin A (ETA) receptor. It has been evaluated in clinical trials for the treatment of prostate cancer and also for the treatment of chronic kidney disease (CKD) associated with Type II diabetes. Data reported from such clinical trials has included, for example, fasting glucose, glycosylated hemoglobin level, triglyceride, lipoprotein-A, and uric acid levels in patients receiving atrasentan as compared with those receiving a placebo. (See, e.g., Raichlin, et al., Efficacy and safety of atrasentan in patients with cardiovascular risk and early atherosclerosis. Hypertension; 52: 522-528 (2008)).
Notably, to-date there has been no reporting of clinically significant or therapeutically beneficial effects of atrasentan on low-density lipoprotein (LDL) cholesterol levels in patients receiving it. Inasmuch as the relationship between cholesterol levels, and in particular LDL cholesterol levels, and cardiovascular risk in general, and coronary artery disease in particular, is well recognized, a need continues to exist for additional therapies for reducing cholesterol levels, such as the methods of treatment using atrasentan, as discussed below.